A Comparative Analysis of Fibroblast Activation Protein-Targeted Small Molecule–Drug, Antibody–Drug, and Peptide–Drug Conjugates
Aureliano Zana, Claudia Puig-Moreno, Matilde Bocci, Ettore Gilardoni, Cesare Di Nitto, Lucrezia Principi, Domenico Ravazza, Giulia Rotta, Eleonora Prodi, Roberto De Luca, Dario Neri, Samuele Cazzamalli
Abstract
comparative evaluation of chemically defined antibody-drug conjugates (ADCs), small molecule-drug conjugates (SMDCs), and peptide-drug conjugates (PDCs) targeting and activated by fibroblast activation protein (FAP) in solid tumors. Both the SMDC (OncoFAP-Gly-Pro-MMAE) and the ADC (7NP2-Gly-Pro-MMAE) candidates delivered high amounts of active payload (i.e., MMAE) selectively at the tumor site, thus producing a potent antitumor activity in a preclinical cancer model.
Topics & Concepts
ChemistryDrugPeptideConjugateFibroblast activation protein, alphaSmall moleculeAntibody-drug conjugateIn vivoPharmacologyAntibodyCombinatorial chemistryBiochemistryCancerMonoclonal antibodyImmunologyBiotechnologyMathematicsBiologyInternal medicineMathematical analysisMedicinePeptidase Inhibition and AnalysisNeuroendocrine Tumor Research AdvancesRadiopharmaceutical Chemistry and Applications